Assay Detail
Binding
CHEMBL3593136
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.54 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590107 | — | — | 1 | 8.40 |
| CHEMBL3590120 | — | — | 1 | 8.17 |
| CHEMBL3590118 | — | — | 1 | 7.72 |
| CHEMBL3590121 | — | — | 1 | 7.66 |
| CHEMBL3590123 | — | — | 1 | 7.32 |
| CHEMBL3590125 | — | — | 1 | 7.18 |
| CHEMBL3590124 | — | — | 1 | 7.14 |
| CHEMBL3590117 | — | — | 1 | 6.92 |
| CHEMBL3590110 | — | — | 1 | 6.92 |
| CHEMBL3590122 | — | — | 1 | 6.77 |
| CHEMBL3590109 | — | — | 1 | 6.62 |
| CHEMBL3590111 | — | — | 1 | 6.42 |
| CHEMBL3590108 | — | — | 1 | 5.80 |
| CHEMBL3590116 | — | — | 1 | 5.68 |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | 5.39 |
| CHEMBL3590115 | — | — | 1 | 5.12 |
| CHEMBL3590114 | — | — | 1 | 5.06 |
| CHEMBL3590113 | — | — | 1 | 5.00 |
| CHEMBL3590112 | — | — | 1 | 5.00 |
| CHEMBL3590119 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590107 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3590120 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3590118 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3590121 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3590123 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3590125 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3590124 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3590117 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3590110 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3590122 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3590109 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3590111 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3590108 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3590116 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3590106 | ULIXERTINIB | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3590115 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3590114 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3590113 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590112 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590119 | — | IC50 | > | 30000.0 | nM | - |